Hexarelin: what the studies show, status and safety
Summary
Hexarelin is a lab-made peptide of six building blocks that prompts the pituitary gland to release growth hormone, by docking onto the receptor for the hunger hormone ghrelin. Researchers in Milan and Argenteuil described it in 1994, and more than a hundred papers went on to test it in people. Almost all of them gave one dose and measured a hormone level, and the single study that treated adults for four months found no change in the growth factor IGF-I, in body fat, in lean mass or in bone. No country has ever approved it, and the world anti-doping list names it.
Key findings at a glance
- Sixteen weeks of treatment changed nothing that can be seen or felt. In 12 older adults injecting twice daily, the growth factor IGF-I stayed put (p = 0.24), as did body fat (p = 0.6), lean mass (p = 0.3) and bone density (p = 0.3) [1].
- It is not a selective peptide, and never was. In healthy adults the rise in the trigger hormone ACTH matched what hCRH produces, the natural hormone used in hospital to test the adrenal glands [2]. Prolactin levelled off 180 percent above its starting value [3].
- How much reaches the blood depends heavily on the route. Under the skin 77.0 ± 10.5 percent, through the nose 4.8 ± 0.9 percent, swallowed 0.3 ± 0.1 percent [4].
- The heart effect stopped where the illness was worst. In dilated cardiomyopathy the pumping fraction did not move (16.7 ± 2.1 to 17.7 ± 1.7 percent). In ischaemic cardiomyopathy it rose from 22.6 ± 2.1 to 26.2 ± 2.5 percent (p < 0.05) [5].
- Named on the anti-doping list under both of its names. Section S2.2.4 of the 2026 Prohibited List reads "examorelin (hexarelin)", banned at all times [6].
- In Australia, possessing it without authority is illegal. The Poisons Standard lists it as prescription-only and again in the appendix that carries that rule [7].
- Zero registered trials, and well over a hundred papers. ClinicalTrials.gov returns nothing at all [8], while a literature search returns 313 records, 138 of them from 1994 to 2000 [9].
What it is
Hexarelin is a synthetic peptide of six building blocks. It is not a hormone, and it is not a fragment of any protein the body makes. Romano Deghenghi described it in 1994 with pharmacologists at the University of Milan, and it has carried two development codes ever since, EP-23905 and MF-6003 [10]. It has no brand name, because no country ever licensed a product containing it.
It was built from the older peptide GHRP-6 by changing one building block. The tryptophan in second position was swapped for a methylated version, which enzymes find harder to cut apart. Deghenghi described that swap as the step that made peptides of this family work when swallowed, although absorption still rarely passed 1 percent of the dose given [11].
Quick facts
| Field | Value | Ref |
|---|---|---|
| Generic name | Examorelin, the official international name for the same substance | [12] |
| Development codes | EP-23905, MF-6003 | [12] |
| Class | Growth hormone releasing peptide, switching on the ghrelin receptor | [10], [11] |
| Sequence | His-D-2-methyl-Trp-Ala-Trp-D-Phe-Lys-NH2 | [12] |
| Structure | Six building blocks, capped at one end, two of them mirror images, one not found in proteins | [11], [12] |
| Formula and mass | C47H58N12O6, 887.0 g/mol | [12] |
| How long it lasts in people | Never measured directly; the growth hormone rise fades with a half-life of about 55 minutes | [13] |
| How long it lasts in animals | 120 minutes in dogs, 75.9 ± 9.3 minutes in rats | [14], [15] |
| Status | Human studies stopped after 2004, approved nowhere | [8], [9] |
| Discoverer | Romano Deghenghi, Europeptides, with the University of Milan | [10], [11] |
| CAS registry number | 140703-51-1, free base | [12] |
| PubChem CID | 6918297 | [12] |
| UNII | 09QF37C617 | [12] |
| DrugBank | DB19510 | [16] |
| Entry in an official reference book | None | [12] |
How it works
Hexarelin docks onto the receptor for the hunger hormone ghrelin, and most of what follows comes from that single action [10].
- The pituitary, by way of the hypothalamus. The signal does not reach the pituitary on its own. In patients whose link between hypothalamus and pituitary had been physically cut, the growth hormone response was absent; where the deficiency had no anatomical cause, it was intact [17].
- The stress hormone axis, through a different messenger. In 15 healthy men, adding the natural hormone CRH enlarged the ACTH response, from 3444 ± 696 to 6580 ± 1572 ng/l × 125 min (p = 0.01), and the cortisol response from 45,844 ± 2925 to 63,170 ± 2616 nmol/l × 125 min (p = 0.001). Desmopressin, a vasopressin-like drug, changed neither (3540 ± 852 ng/l × 125 min). The authors concluded that vasopressin carries part of the signal [18].
- A second, separate target in the heart. A binding protein of 84,000 daltons was pulled from rat heart membranes, and its sequence proved to be rat CD36. In mice bred without CD36, the peptide no longer tightened the coronary vessels [19], [20].
- That heart target is not the pituitary receptor. Two other potent growth hormone releasers, MK-0677 and EP 51389, did not displace hexarelin from the heart binding sites and produced no vessel response at all [20].
- Protection that may not need growth hormone. In rats whose pituitary had been removed, hexarelin still limited the damage from blocked and restored blood flow, much as growth hormone did. EP 51389 did nothing [21].
- A hand in fat metabolism. In fat cells and mice, activating CD36 switched on genes for mitochondria and burning fat. The effect disappeared in mice without CD36 [22].
One distinction is worth holding on to. Ipamorelin, of the same family, was called the first selective one, because the stress hormones stayed flat far above the effective dose [23]. Hexarelin does not behave that way, and that difference runs through everything below.
What the studies found
Growth hormone release
Phase 1 Twelve healthy men received 0.5, 1 and 2 micrograms per kilogram into a vein, along with a dummy injection, without knowing which was which. Peak growth hormone was 3.9, 26.9, 52.3 and 55.0 ng/ml, rising about 30 minutes after the injection and back to baseline within 240 minutes [13]. Half the maximum effect came at 0.50 µg/kg, and the highest dose was already close to the ceiling.
The response depends on who receives it. Across 60 people it was strongest during puberty, at 1960.2 ± 283.5 µg·min/l, against 769.5 ± 122.2 before puberty, 1829.7 ± 243.1 in young adults and 951.1 ± 232.9 in old age [24]. A study of 96 children found the same pattern, 77.5 ± 8.5 against 39.4 ± 4.4 µg/l (p < 0.001) [25].
Body fat matters as well. In 21 older adults it was the strongest single predictor: the more of it, the smaller the response (r = -0.72, p = 0.0001) [26].
How it is given
Phase 1 Twelve volunteers received the peptide by all four routes in the same study. Measured against injection into a vein, 77.0 ± 10.5 percent of the effect survived injection under the skin, 4.8 ± 0.9 percent survived the nose, and 0.3 ± 0.1 percent survived swallowing [4]. Twenty micrograms per kilogram sprayed into the nose matched 1 µg/kg into a vein.
Biological availability in 12 healthy volunteers, measured against injection into a vein. Swallowing needed 20 to 40 mg to match 1 microgram per kilogram given intravenously. Source [4].
The hormones that rise alongside
Phase 1 In 12 healthy adults, ACTH rose from 16.3 ± 7.2 to 32.4 ± 17.7 pg/ml (p < 0.005) and cortisol from 110.0 ± 31.6 to 135.9 ± 51.0 µg/l (p < 0.01). Both responses were comparable to those produced by hCRH, the hormone used clinically for exactly this test, which lifted ACTH from 17.1 ± 7.7 to 35.7 ± 13.2 pg/ml (p < 0.01) [2]. Seventeen patients with Cushing's syndrome were studied alongside them, and the picture split by cause. Where the cause lay in the pituitary, hexarelin raised ACTH about sevenfold more than hCRH did (p < 0.02) and cortisol about fourfold more (p < 0.05). Where it lay in an adrenal adenoma or in ectopic ACTH, neither hormone moved at all [2].
A dose-response study filled in the shape of it. Prolactin levelled off at 180 percent above baseline, with half the effect at 0.39 ± 0.02 µg/kg. Cortisol climbed in steps to roughly 40 percent above baseline once the dose passed 0.5 µg/kg [3]. A head-to-head comparison with GHRP-2 found the two peptides alike on every one of these measures [27].
Sixteen weeks in older adults
Phase 1/2 This is the study that matters most, and it is negative. Twelve healthy older adults injected 1.5 µg/kg under the skin twice a day for 16 weeks. The growth hormone released fell from 19.1 ± 2.4 to 12.3 ± 2.4 µg/l·h by week 4 (p < 0.05) and 10.5 ± 1.8 by week 16 (p < 0.01), then returned to 19.4 ± 3.7 four weeks after stopping [1], [28].
Nothing downstream moved. IGF-I and its carrier protein IGFBP-3 were unchanged (p = 0.24 and p = 0.74). So were body fat, lean mass and bone density (p = 0.6, p = 0.3, p = 0.3). Only one bone marker rose (p = 0.019) [1]. The authors called the effect on the growth hormone axis minimal.
Twelve healthy older adults, 1.5 micrograms per kilogram under the skin twice daily. The response fades and then recovers after stopping. Across the same 20 weeks, IGF-I, body fat, lean mass and bone density did not change. Source [1].
Children with short stature
Phase 2 Eight children between 4 and 11.6 years old were sprayed 60 µg/kg into the nose three times daily for up to eight months. IGF-I rose from 10.4 ± 3.9 to 14.1 ± 4.6 nmol/l (p < 0.004) and growth speed from 5.3 ± 0.8 to 8.3 ± 1.7 cm per year (p < 0.0001) [29]. A parallel study of seven children found 5.3 ± 0.9 rising to 7.4 ± 1.6 cm per year (p < 0.005) [30].
Neither study had a control group, neither assigned children at random, and neither followed anyone to adult height. Without a comparison group, catch-up growth cannot be separated from the ordinary course of things. In the same seven children the growth hormone response to a nasal test dose fell from 70.6 ± 28.2 to 34.1 ± 15.7 mU/l within seven days (p < 0.002), stayed near that level at 37.5 ± 10.3 over six months (p < 0.03), and recovered to 42.1 ± 4.7 three months after treatment ended (p < 0.005) [30].
The heart
Phase 1/2 In seven healthy men, a single injection lifted the pumping fraction of the left ventricle from 64.0 ± 1.5 to 70.7 ± 3.0 percent (p < 0.03), peaking at 30 minutes and falling back by 60. Growth hormone given in its own right, in the same study and raising blood levels just as high, changed nothing [31]. In seven men with growth hormone deficiency the fraction rose from 50 ± 1 to 57 ± 2 percent [32].
Phase 2 Twenty-four men with coronary disease were studied under anaesthesia during bypass surgery. Hexarelin raised the pumping fraction, cardiac index and output from 10 minutes to 90 minutes (p < 0.001) and lowered the wedge pressure (p < 0.01). Growth hormone, the natural releasing hormone GHRH and a dummy injection did nothing measurable [33].
The heart result that failed
Phase 2 Thirteen patients with severe heart failure were given a single injection. In the five with ischaemic cardiomyopathy the pumping fraction rose from 22.6 ± 2.1 to 26.2 ± 2.5 percent (p < 0.05). In the eight with dilated cardiomyopathy, the group with the weakest hearts, it did not move at all: 16.7 ± 2.1 against 17.7 ± 1.7 percent [5]. Growth hormone rose to the same degree in both groups.
An earlier study of 12 patients with severe dilated cardiomyopathy found the same absence [34]. The effect and the growth hormone rise come apart in both directions, and the effect fails in the patients who would need it most.
Sleep
Phase 1 Seven young volunteers received four injections of 50 micrograms across the evening. Stage four sleep in the first half of the night fell significantly, as did the delta power of the recording across the whole night. Growth hormone and prolactin rose all night, ACTH and cortisol in the first half [35]. That is the opposite of what ghrelin and GHRH do.
As a hospital test
Phase 2 This is the one use for which hexarelin was ever seriously developed, and even here it did not reach approval. In 19 patients, growth hormone peaks were higher than after insulin-induced low blood sugar (67.1 ± 16 against 26.9 ± 6.8 mU/l, p < 0.001), while cortisol peaks were lower (420 ± 34 against 605 ± 50 nmol/l, p < 0.001) [36]. As a test of adrenal reserve the authors ruled it out.
A low dose combined with GHRH separated patients cleanly: 83.6 ± 4.5 µg/l in healthy adults against 2.6 ± 0.7 µg/l in adults with growth hormone deficiency [37].
What is still unknown
- Any clinical outcome at all. No randomised controlled study has measured survival, symptoms, strength or quality of life, in any condition [8], [9].
- Anything past 16 weeks. That is the longest anyone has been treated, in any population [1].
- Use by healthy adults for muscle or fat. The only multi-month adult study measured body composition and found no change [1].
- Pregnancy, breastfeeding and fertility. No data of any kind.
- Cancer risk, genetic damage and immune reactions. No regulatory testing programme was ever run, so none of it is publicly documented.
Side effects and safety
No authority has ever weighed the benefits against the risks, because no application was ever filed. Everything below comes from small investigator-run studies of the 1990s, which did not collect side effects in a structured way. Statements that it was well tolerated should be read in that light.
What was measured, in people:
- Cortisol up by roughly 40 percent above baseline once the dose passed 0.5 µg/kg, and from 110.0 ± 31.6 to 135.9 ± 51.0 µg/l at 2 µg/kg [2], [3].
- ACTH roughly doubled, from 16.3 ± 7.2 to 32.4 ± 17.7 pg/ml (p < 0.005). Where Cushing's syndrome arises in the pituitary, the rise outran the one produced by hCRH about sevenfold, so the reaction is not predictable when the adrenal axis is diseased [2].
- Prolactin up by 180 percent, evenly across every age group tested [3], [24].
- Less deep sleep, in seven young volunteers given four evening injections [35].
- A weaker response over time, down to about 55 percent after 16 weeks and back to baseline four weeks after stopping [1], [30].
- A short dip in the thyroid signal TSH in children, from 1.0 ± 0.26 to 0.64 ± 0.2 mU/l through the nose (p < 0.005) and from 1.0 ± 0.3 to 0.7 ± 0.3 mU/l into a vein (p < 0.05), with free T4 and T3 unchanged and all values inside the normal range [38].
- No acute complaints reported in several studies of children and older adults, none of which used a structured questionnaire [39], [40].
Two further risks come from the wider family rather than from hexarelin itself. A review of growth hormone releasers names rising blood sugar, through reduced insulin sensitivity, as the main safety reservation for the class [41]. In obese rats treated for 30 days, insulin and blood sugar both rose [42].
Appetite is the second. In 15 healthy men a rating scale showed a small acute increase [18], and in dogs and rats the effect is clear and follows the dose [43], [44].
Some cautions follow directly from the studies rather than from a label, since no label exists. Where Cushing's syndrome starts in the pituitary, the ACTH and cortisol response overshoots badly; where it starts in an adrenal adenoma or in ectopic ACTH, it vanishes entirely [2]. Where the hypothalamus and pituitary have been physically separated, there is no growth hormone response [17]. In obesity the response is blunted [26].
One animal finding sits oddly beside the human heart results and was never resolved. In isolated rat hearts, hexarelin tightened the coronary vessels as the dose rose. The authors asked openly whether CD36 might carry the coronary spasm seen in atherosclerosis [19], [20]. Nobody has looked at that in people.
The record also carries a warning about what is sold. On 8 December 2025 the FDA cited a United States bulk ingredient firm over its official listing for "Hexarelin Acetate" (NDC 71052-621). The underlying filing named a different active ingredient, a peptide coded B27PD, and the agency classed the product as misbranded [45].
Doses used in studies
The doses below are simply what the cited studies gave, listed so that the results can be understood. They are not advice on how to use anything. Most human entries are single test doses given in hospital under supervision, and animal doses cannot be scaled to people.
| Study | Model | Dose | Route | Frequency | Duration | Ref |
|---|---|---|---|---|---|---|
| Imbimbo 1994, dose and response | 12 healthy men | 0.5, 1, 2 µg/kg, plus dummy | Into a vein | Once per level | Once | [13] |
| Ghigo 1994, four routes | 12 healthy volunteers | 1 and 2 µg/kg; 1.5 and 3 µg/kg; 20 µg/kg; 20 and 40 mg | Vein, skin, nose, mouth | Once per route | Once | [4] |
| Massoud 1996, dose and response | Healthy adult men | 0 to 1.0 µg/kg; 0.125 µg/kg with GHRH | Into a vein | Once | Once | [3] |
| Arvat 1997, age comparison | 60 people, children to elderly | 1.0 and 2.0 µg/kg | Into a vein | Once | Once | [24], [27] |
| Loche 1995, children | 45 short, 10 obese, 5 with pituitary damage | 2 µg/kg | Into a vein | Once | Once | [40] |
| Bellone 1995, before and during puberty | 96 children, 4.1 to 17.4 years | 1.0 and 2.0 µg/kg; 10 mg by mouth | Vein, mouth | Once | Once | [25] |
| Laron 1994, nose against vein | 10 children, 2 adults | 1 µg/kg; 20 µg/kg | Vein, nose | Once per test | Once | [38] |
| Laron 1995, continued treatment | 8 short children, 4 to 11.6 years | 60 µg/kg | Into the nose | Three times daily | Up to 8 months | [29] |
| Klinger 1996, fading response | 7 short children | 60 µg/kg; test doses 20 µg/kg and 1 µg/kg | Nose, and vein for tests | Three times daily | 6 to 10 months | [30] |
| Rahim 1998, 16 weeks | 12 healthy older adults | 1.5 µg/kg | Under the skin | Twice daily | 16 weeks, follow-up to week 20 | [1], [46] |
| Maccario 2002, 24-hour profile | 6 young men | 1.5 µg/kg; test dose 1 µg/kg | Under the skin | Two or three times daily | 24 hours | [47] |
| Ghigo 1996, short courses in ageing | 7 older adults; 7 older women | 1.25 mg into the nose; 20 mg by mouth | Nose, mouth | Three times daily | 8 days; 15 days | [39] |
| Frieboes 2004, sleep | 7 young volunteers | 4 × 50 µg, total 200 µg | Into a vein | Hourly from 22:00 | One night | [35] |
| Gasperi 1999, diagnostic test | 25 to 33 healthy adults, 19 with deficiency | 0.25 µg/kg with 1 µg/kg GHRH | Into a vein | Once | Once | [37] |
| Jenkins 1999, dialysis patients | 18 on dialysis, 6 healthy | 1 and 2 µg/kg | Into a vein | Once | Once | [48] |
| Roumi 1995, dog pharmacokinetics | Dogs | 1 µg/kg; 1, 10, 100 µg/kg | Vein, skin | Once | Once | [15] |
| Roumi 2000, rat pharmacokinetics | Male rats | 5 µg/kg; 5, 10, 50 µg/kg | Vein, skin | Once | Once | [14] |
| Locatelli 1999, rat without pituitary | Rats | 80 µg/kg | Under the skin | Daily | 7 days | [21] |
| Tivesten 2000, rat after heart attack | Rats | 10 or 100 µg/kg per day | Under the skin | Twice daily | 2 weeks | [49] |
| Cella 1996, aged dogs | 6 old beagles | 500 µg/kg per day | Under the skin | Daily | 16 weeks in three blocks | [50] |
| De Gennaro-Colonna 2000, obese rats | Obese and lean rats | 80 µg/kg | Under the skin | Twice daily | 30 days | [42] |
| Zhang 2018, diabetic rats | Diabetic rats | 100 µg/kg | Under the skin | Daily | 2 weeks | [51] |
A review of 2026 set these study doses beside what circulates in bodybuilding forums: 100 to 200 micrograms under the skin, once or twice a day, over 8 to 12 weeks. Its authors describe that as unregulated practice drawn from commercial websites, not as guidance [52]. It runs for months where the studies ran for a day.
Development and approval status
From first description to named prohibition
- 1994First described in Milan and ArgenteuilBuilt from GHRP-6 by changing one building block, ref [10]
- 1994First human studies: dose and response, and all four routes12 healthy men each, refs [4], [13]
- 1995 to 1996Children with short stature treated through the noseGrowth speeds up, and the response fades within 7 days, refs [29], [30]
- 1998Sixteen weeks in older adults changes nothing downstreamIGF-I, body fat, lean mass and bone density all unmoved, ref [1]
- 1999 to 2002Heart studies find an effect lasting about an hourGrowth hormone itself produced none, refs [31], [33]
- 2002The effect fails in dilated cardiomyopathyPumping fraction 16.7 to 17.7 percent, not significant, ref [5]
- 2004Last human study published, on sleepHuman research effectively stops here, refs [9], [35]
- 2025FDA warning letter over a listing for hexarelin acetate on 8 DecemberFiling named a different active ingredient, ref [45]
- 2026Named on the anti-doping list and in the Australian Poisons StandardBanned at all times, and possession without authority is illegal, refs [6], [7]
- 1994 — the first description appears in Life Sciences, from Europeptides and the University of Milan [10].
- 1994 to 1996 — the human programme runs fast: dose-response, all four routes, children before and during puberty, older adults [4], [13], [25], [39].
- 1998 — the only multi-month adult study reports no change in IGF-I or body composition [1].
- 1999 to 2002 — the heart studies find an effect lasting about an hour, then fail in the sickest group [5], [31], [33].
- 2004 — the last human study is published, and the substance disappears from clinical research [9], [35].
- 2026 — it stands named on the anti-doping list, in German anti-doping law and in the Australian Poisons Standard [6], [7], [53].
Why the programme stopped is not documented in any source read for this page. Four findings stood in the way of further development: the missing selectivity, the fading response, the absent IGF-I rise over four months and an oral availability of 0.3 percent [1], [2], [4], [11]. Whether any of them caused the decision is unknown, and this page does not claim it.
| Market | Status | Note | Ref |
|---|---|---|---|
| United States | Not approved | No label; not on either compounding list | [54], [55], [56] |
| European Union | Not approved | Register search blocked; no authorisation known | [52], [57] |
| Germany | Not approved | Named in the anti-doping annex | [53] |
| United Kingdom | Not approved | Register search returned no usable page | [58] |
| Australia | Prescription-only | Possession without authority is illegal | [7] |
| Canada | Not approved | No entry in the database | [59] |
| Russia | Unknown | Register returned nothing, including for the control query | [60] |
Every query behind this table was run on 10 September 2026, and three rows deserve a caveat. The European, British and Russian registers could not be searched properly that day [57], [58], [60]. Those rows rest on something weaker: no brand name for hexarelin appears anywhere in the literature since 1994.
The American row carries a different caution. Hexarelin appears neither among the substances nominated for pharmacy compounding nor among those flagged as a possible safety risk [55], [56]. Ipamorelin appears ten times on the second page, so the search works. The absence means no decision has been taken, not that anyone has judged it safe.
Australia is the outlier. The Poisons Standard of June 2026 lists HEXARELIN in Schedule 4 and again as item 22 of the table under Appendix D, clause 5 [7]. That clause is headed with the rule that possessing these substances without authority is illegal, and section 64(4) of the instrument states it directly.
Anti-doping
Hexarelin is banned in sport at all times, in and out of competition, and counts as a non-specified substance, the stricter of the two categories. It is printed on the list by name rather than caught by a general clause.
Section S2.2.4 of the 2026 Prohibited List reads: "GH-releasing peptides (GHRPs) e.g. alexamorelin, examorelin (hexarelin), GHRP-1, GHRP-2 (pralmorelin), GHRP-3, GHRP-4, GHRP-5 and GHRP-6" [6]. Both names appear together, which matters, because checking only one of them can return nothing. Germany names it in the annex to its anti-doping law, alongside GHRP-2 and GHRP-6 [53].
Testing for it is established. Validated mass-spectrometry methods detect the peptide and its fragments in urine, with detection limits of 0.2 to 1 ng/ml [61]. In an excretion study after nasal dosing, one fragment remained detectable after the peptide itself had gone [62]. The wider picture for this family is at peptides banned in sport.
Compared with related peptides
| Peptide | Class | Approval | Anti-doping | Distinguishing finding |
|---|---|---|---|---|
| Hexarelin | Growth hormone releasing peptide | None, anywhere | Named, S2.2.4 [6] | Raises ACTH as strongly as hCRH does [2] |
| Ipamorelin | Growth hormone secretagogue | None, anywhere | Named, S2.2.4 [6] | The stress hormones stayed flat in pigs above 200 times the effective dose [23] |
| GHRP-2 and GHRP-6 | Growth hormone releasing peptides | None, anywhere | Named, S2.2.4 [6] | GHRP-2 matched hexarelin on every hormone measured in people [27]; GHRP-6 differs by a single building block [10] |
| Ibutamoren (MK-677) | Not a peptide, same receptor | None in the FDA database [63] | Named, S2.2.4 [6] | Did not displace hexarelin from the binding sites in rat heart [20] |
| Tesamorelin | Copy of the natural releasing hormone GHRH | Approved, licence BLA 022505 [63] | Named, S2.2.4 [6] | The only approved medicine in this table |
| CJC-1295 | Copy of the natural releasing hormone GHRH | None in the FDA database [63] | Named, S2.2.4 [6] | The anti-doping list groups it with the GHRH analogues, not with the ghrelin-receptor peptides [6] |
Two lines run through this table. The first divides the peptides that copy the natural releasing hormone GHRH from those that act on the ghrelin receptor. Hexarelin released roughly twice as much growth hormone as GHRH did, 3175 ± 506 against 1544 ± 161 µg·min/l (p < 0.001) [4].
The second runs through the ghrelin group itself, and it is about selectivity. Ipamorelin was built to leave the stress hormones alone [23]; hexarelin does the opposite, by design and by measurement [2], [3]. Treating the two as interchangeable misses the most consistent finding in this literature.
Common misconceptions
- "Hexarelin and GHRP-6 are basically the same thing." They differ at one position, and that position is the entire development step. A methyl group on the tryptophan makes the molecule harder for enzymes to cut. In rats they were equally potent into a vein, while under the skin hexarelin lasted longer [10], [11].
- "Hexarelin and ipamorelin are interchangeable growth hormone peptides." Ipamorelin left ACTH and cortisol untouched in pigs above 200 times its effective dose [23]. Hexarelin raises prolactin, ACTH and cortisol in people, in step with the dose [2], [3].
- "It is proven to protect the human heart." What is proven is that one injection lifts a pumping measurement for about an hour [31], [33]. No study has ever measured a clinical outcome, and in dilated cardiomyopathy even the measurement did not move [5]. The protection findings come from rats and mice [21].
- "Examorelin is a different, related substance." It is the same substance under its official generic name. One database entry covers both, and the anti-doping list prints them together as "examorelin (hexarelin)" [6], [12].
- "With no registered trials, it was never properly studied in people." The opposite. The registry holds nothing because the studies predate the registration rules [8], and the literature holds 313 records [9]. The fair criticism is the shape of those studies, not their number: single doses, hormone levels, few control groups.
- "The effect fades, so you just need breaks." The fading is real, partial and reversible [1], [30]. But in the four-month adult study the remaining response still produced no change in IGF-I, body fat, lean mass or bone [1]. Timing the breaks differently does not fix that result.
- "The children's studies show it builds muscle in adults." Those studies covered eight and seven short children, with no control group and under a year of follow-up [29], [30]. The one multi-month adult study measured body composition directly and found nothing [1].
- "What is sold as hexarelin is hexarelin." Nobody has published an analysis of grey-market material. Peptides of this class do turn up in products sold as supplements, where about 50 micrograms of GHRP-2 per tablet were once measured [64].
Frequently asked questions
Is hexarelin approved anywhere?
No. No country has licensed it as a medicine, for any condition. It has an official generic name, examorelin, and it has never had a brand name, because no product containing it was ever authorised. The register searches behind this page were run on 10 September 2026.
What is hexarelin?
It is a lab-made peptide of six building blocks, written as His-D-2-methyl-Trp-Ala-Trp-D-Phe-Lys-NH2. It switches on the receptor for the hunger hormone ghrelin and thereby sets off a burst of growth hormone. It was built from the older peptide GHRP-6 by changing a single building block.
Did hexarelin work in the studies?
It reliably released growth hormone, and that is the finding that holds up. What it did not do is change anything downstream. Over 16 weeks in 12 older adults, the growth factor IGF-I did not move (p = 0.24), and neither did body fat (p = 0.6), lean mass (p = 0.3) or bone density (p = 0.3).
Does hexarelin raise cortisol and prolactin?
Yes, and this is its defining feature. In healthy adults the rise in the trigger hormone ACTH matched the rise produced by hCRH, the natural hormone used in hospital to test the adrenal glands. Prolactin levelled off at 180 percent above its starting value. Ipamorelin was developed precisely to avoid this.
Is hexarelin good for the heart?
That claim rests on a measurement, not on an outcome. A single injection into a vein lifted the heart's pumping fraction for about an hour in healthy people and in several patient groups. In the sickest group, those with dilated cardiomyopathy, it did nothing at all. No study has ever measured survival, symptoms or hospital admissions.
What are the known side effects of hexarelin?
The measured ones are hormonal: cortisol up by about 40 percent, prolactin up by 180 percent, and the trigger hormone ACTH roughly doubled. One sleep study found less deep sleep. Beyond that the record is thin, because these small studies of the 1990s never collected side effects in a structured way.
Is hexarelin banned in sport?
Yes, at all times, in and out of competition. Section S2.2.4 of the 2026 Prohibited List names it under both of its names, as "examorelin (hexarelin)", among the growth hormone releasing peptides. It counts as a non-specified substance, the stricter of the two categories.
Is hexarelin legal to possess in Australia?
No, not without authority. The Poisons Standard of June 2026 lists HEXARELIN as prescription-only and again in an appendix headed with the rule that possessing these substances without authority is illegal. Germany names it in the annex to its anti-doping law.
Why does the effect of hexarelin fade with continued use?
The pituitary gland responds less after repeated dosing, but only partly and not permanently. After 16 weeks of twice-daily injections the growth hormone response had fallen to roughly 55 percent, and four weeks after stopping it was back where it started. In children treated through the nose it faded within seven days.
What is still unknown about hexarelin?
Nearly everything that would matter to a person taking it. There is no randomised controlled study with a clinical outcome, in any condition. Nothing is known beyond 16 weeks, nothing about pregnancy, nothing about cancer risk, and nothing about what grey-market material actually contains.
Sources
- Rahim A, O'Neill PA, Shalet SM (1998). Growth hormone status during long-term hexarelin therapy. Journal of Clinical Endocrinology and Metabolism 83(5):1644-1649. PMID 9589671. DOI 10.1210/jcem.83.5.4812
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- World Anti-Doping Agency. The 2026 Prohibited List, in force from 1 January 2026; section S2.2.4, third bullet. Official text as annex to BGBl. III of 30 December 2025, No. 219, page 4 of 11. Full text read 10 September 2026.
- Therapeutic Goods (Poisons Standard—June 2026) Instrument 2026, F2026L00633, registered 28 May 2026. Schedule 4 entry "# HEXARELIN."; Appendix D, clause 5, item 22; index entry; section 64(4). https://www.legislation.gov.au/F2026L00633/asmade
- ClinicalTrials.gov API v2. Queries for "hexarelin", "examorelin" and "EP-23905" by intervention and by term, each returning 0 studies; control queries in the same run returned 749 for semaglutide and 3 for ipamorelin. Retrieved 10 September 2026. https://clinicaltrials.gov/api/v2/studies?query.intr=hexarelin
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- PubChem. Compound CID 6918297, examorelin; formula C47H58N12O6, 887.0 g/mol, CAS 140703-51-1, UNII 09QF37C617, ChEMBL108335, development codes EP-23905 and MF-6003. Retrieved 10 September 2026. https://pubchem.ncbi.nlm.nih.gov/compound/6918297
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- Wikidata. Item Q21098927, examorelin, retrieved via Special:EntityData 10 September 2026; DrugBank identifier DB19510. https://www.wikidata.org/wiki/Q21098927
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- Korbonits M, Kaltsas G, Perry LA, Putignano P, Grossman AB, Besser GM, Trainer PJ (1999). The growth hormone secretagogue hexarelin stimulates the hypothalamo-pituitary-adrenal axis via arginine vasopressin. Journal of Clinical Endocrinology and Metabolism 84(7):2489-2495. PMID 10404825. DOI 10.1210/jcem.84.7.5811
- Bodart V, Febbraio M, Demers A, McNicoll N, Pohankova P, Perreault A, Sejlitz T, Escher E, Silverstein RL, Lamontagne D, Ong H (2002). CD36 mediates the cardiovascular action of growth hormone-releasing peptides in the heart. Circulation Research 90(8):844-849. PMID 11988484. DOI 10.1161/01.res.0000016164.02525.b4
- Bodart V, Bouchard JF, McNicoll N, Escher E, Carrière P, Ghigo E, Sejlitz T, Sirois MG, Lamontagne D, Ong H (1999). Identification and characterization of a new growth hormone-releasing peptide receptor in the heart. Circulation Research 85(9):796-802. PMID 10532947. DOI 10.1161/01.res.85.9.796
- Locatelli V, Rossoni G, Schweiger F, Torsello A, De Gennaro Colonna V, Bernareggi M, Deghenghi R, Müller EE, Berti F (1999). Growth hormone-independent cardioprotective effects of hexarelin in the rat. Endocrinology 140(9):4024-4031. PMID 10465272. DOI 10.1210/endo.140.9.6948
- Rodrigue-Way A, Demers A, Ong H, Tremblay A (2007). A growth hormone-releasing peptide promotes mitochondrial biogenesis and a fat burning-like phenotype through scavenger receptor CD36 in white adipocytes. Endocrinology 148(3):1009-1018. PMID 17138655. DOI 10.1210/en.2006-0975
- Raun K, Hansen BS, Johansen NL, Thøgersen H, Madsen K, Ankersen M, Andersen PH (1998). Ipamorelin, the first selective growth hormone secretagogue. European Journal of Endocrinology 139(5):552-561. PMID 9849822. DOI 10.1530/eje.0.1390552
- Arvat E, Ramunni J, Bellone J, Di Vito L, Baffoni C, Broglio F, Deghenghi R, Bartolotta E, Ghigo E (1997). The GH, prolactin, ACTH and cortisol responses to Hexarelin, a synthetic hexapeptide, undergo different age-related variations. European Journal of Endocrinology 137(6):635-642. PMID 9437229. DOI 10.1530/eje.0.1370635
- Bellone J, Aimaretti G, Bartolotta E, Benso L, Imbimbo BP, Lenaerts V, Deghenghi R, Camanni F, Ghigo E (1995). Growth hormone-releasing activity of hexarelin, a new synthetic hexapeptide, before and during puberty. Journal of Clinical Endocrinology and Metabolism 80(4):1090-1094. PMID 7714074. DOI 10.1210/jcem.80.4.7714074
- Rahim A, O'Neill PA, Shalet SM (1998). The effect of body composition on hexarelin-induced growth hormone release in normal elderly subjects. Clinical Endocrinology (Oxford) 49(5):659-664. PMID 10197083. DOI 10.1046/j.1365-2265.1998.00586.x
- Arvat E, di Vito L, Maccagno B, Broglio F, Boghen MF, Deghenghi R, Camanni F, Ghigo E (1997). Effects of GHRP-2 and hexarelin, two synthetic GH-releasing peptides, on GH, prolactin, ACTH and cortisol levels in man. Comparison with the effects of GHRH, TRH and hCRH. Peptides 18(6):885-891. PMID 9285939. DOI 10.1016/s0196-9781(97)00016-8
- Rahim A, Shalet SM (1998). Does desensitization to hexarelin occur? Growth Hormone and IGF Research 8 Suppl A:141-143. PMID 10990150. DOI 10.1016/s1096-6374(98)80039-7
- Laron Z, Frenkel J, Deghenghi R, Anin S, Klinger B, Silbergeld A (1995). Intranasal administration of the GHRP hexarelin accelerates growth in short children. Clinical Endocrinology (Oxford) 43(5):631-635. PMID 8548949. DOI 10.1111/j.1365-2265.1995.tb02929.x
- Klinger B, Silbergeld A, Deghenghi R, Frenkel J, Laron Z (1996). Desensitization from long-term intranasal treatment with hexarelin does not interfere with the biological effects of this growth hormone-releasing peptide in short children. European Journal of Endocrinology 134(6):716-719. PMID 8766941. DOI 10.1530/eje.0.1340716
- Bisi G, Podio V, Valetto MR, Broglio F, Bertuccio G, Del Rio G, Arvat E, Boghen MF, Deghenghi R, Muccioli G, Ghigo E (1999). Acute cardiovascular and hormonal effects of GH and hexarelin, a synthetic GH-releasing peptide, in humans. Journal of Endocrinological Investigation 22(4):266-272. PMID 10342360. DOI 10.1007/BF03343555
- Bisi G, Podio V, Valetto MR, Broglio F, Bertuccio G, Aimaretti G, Pelosi E, Del Rio G, Muccioli G, Ong H, Boghen MF, Deghenghi R, Ghigo E (1999). Cardiac effects of hexarelin in hypopituitary adults. European Journal of Pharmacology 381(1):31-38. PMID 10528131. DOI 10.1016/s0014-2999(99)00537-3
- Broglio F, Guarracino F, Benso A, Gottero C, Prodam F, Granata R, Avogadri E, Muccioli G, Deghenghi R, Ghigo E (2002). Effects of acute hexarelin administration on cardiac performance in patients with coronary artery disease during by-pass surgery. European Journal of Pharmacology 448(2-3):193-200. PMID 12144941. DOI 10.1016/s0014-2999(02)01934-9
- Broglio F, Benso A, Valetto MR, Gottero C, Quaranta L, Podio V, Arvat E, Bobbio M, Bisi G, Ghigo E (2001). Growth hormone-independent cardiotropic activities of growth hormone-releasing peptides in normal subjects, in patients with growth hormone deficiency, and in patients with idiopathic or ischemic dilated cardiomyopathy. Endocrine 14(1):105-110. PMID 11322491. DOI 10.1385/ENDO:14:1:105
- Frieboes RM, Antonijevic IA, Held K, Murck H, Pollmächer T, Uhr M, Steiger A (2004). Hexarelin decreases slow-wave sleep and stimulates the secretion of GH, ACTH, cortisol and prolactin during sleep in healthy volunteers. Psychoneuroendocrinology 29(7):851-860. PMID 15177700. DOI 10.1016/S0306-4530(03)00152-5
- Korbonits M, Kaltsas G, Perry LA, Grossman AB, Monson JP, Besser GM, Trainer PJ (1999). Hexarelin as a test of pituitary reserve in patients with pituitary disease. Clinical Endocrinology (Oxford) 51(3):369-375. PMID 10469018. DOI 10.1046/j.1365-2265.1999.00828.x
- Gasperi M, Aimaretti G, Scarcello G, Corneli G, Cosci C, Arvat E, Martino E, Ghigo E (1999). Low dose hexarelin and growth hormone (GH)-releasing hormone as a diagnostic tool for the diagnosis of GH deficiency in adults: comparison with insulin-induced hypoglycemia test. Journal of Clinical Endocrinology and Metabolism 84(8):2633-2637. PMID 10443652. DOI 10.1210/jcem.84.8.5904
- Laron Z, Frenkel J, Gil-Ad I, Klinger B, Lubin E, Wüthrich P, Boutignon F, Lenaerts V, Deghenghi R (1994). Growth hormone releasing activity by intranasal administration of a synthetic hexapeptide (hexarelin). Clinical Endocrinology (Oxford) 41(4):539-541. PMID 7955465. DOI 10.1111/j.1365-2265.1994.tb02589.x
- Ghigo E, Arvat E, Gianotti L, Grottoli S, Rizzi G, Ceda GP, Boghen MF, Deghenghi R, Camanni F (1996). Short-term administration of intranasal or oral Hexarelin, a synthetic hexapeptide, does not desensitize the growth hormone responsiveness in human aging. European Journal of Endocrinology 135(4):407-412. PMID 8921821. DOI 10.1530/eje.0.1350407
- Loche S, Cambiaso P, Carta D, Setzu S, Imbimbo BP, Borrelli P, Pintor C, Cappa M (1995). The growth hormone-releasing activity of hexarelin, a new synthetic hexapeptide, in short normal and obese children and in hypopituitary subjects. Journal of Clinical Endocrinology and Metabolism 80(2):674-678. PMID 7852535. DOI 10.1210/jcem.80.2.7852535
- Sigalos JT, Pastuszak AW (2018). The safety and efficacy of growth hormone secretagogues. Sexual Medicine Reviews 6(1):45-53. PMID 28400207. DOI 10.1016/j.sxmr.2017.02.004
- De Gennaro-Colonna V, Rossoni G, Cocchi D, Rigamonti AE, Berti F, Müller EE (2000). Endocrine, metabolic and cardioprotective effects of hexarelin in obese Zucker rats. Journal of Endocrinology 166(3):529-537. PMID 10974647. DOI 10.1677/joe.0.1660529
- Rigamonti AE, Cella SG, Marazzi N, Müller EE (1999). Six-week treatment with hexarelin in young dogs: evaluation of the GH responsiveness to acute hexarelin or GHRH administration, and of the orexigenic effect of hexarelin. European Journal of Endocrinology 141(3):313-320. PMID 10474131. DOI 10.1530/eje.0.1410313
- Torsello A, Luoni M, Schweiger F, Grilli R, Guidi M, Bresciani E, Deghenghi R, Müller EE, Locatelli V (1998). Novel hexarelin analogs stimulate feeding in the rat through a mechanism not involving growth hormone release. European Journal of Pharmacology 360(2-3):123-129. PMID 9851578. DOI 10.1016/s0014-2999(98)00677-3
- FDA. Warning letter to Darmerica, LLC (716152), 8 December 2025, published 23 December 2025; listing "Hexarelin Acetate", NDC 71052-621, classed as misbranded under section 502(o). Full text read 10 September 2026. https://www.fda.gov/inspections-compliance-enforcement-and-criminal-investigations/warning-letters/darmerica-llc-716152-12082025
- Rahim A, O'Neill PA, Shalet SM (1999). The effect of chronic hexarelin administration on the pituitary-adrenal axis and prolactin. Clinical Endocrinology (Oxford) 50(1):77-84. PMID 10341859. DOI 10.1046/j.1365-2265.1999.00609.x
- Maccario M, Veldhuis JD, Broglio F, Di Vito L, Arvat E, Deghenghi R, Ghigo E (2002). Impact of two or three daily subcutaneous injections of hexarelin, a synthetic growth hormone (GH) secretagogue, on 24-h GH, prolactin, adrenocorticotropin and cortisol secretion in humans. European Journal of Endocrinology 146(3):310-318. PMID 11888836. DOI 10.1530/eje.0.1460310
- Jenkins RC, El Nahas AM, Wilkie ME, Brown CB, Jones RG, Ghigo E, Ross RJ (1999). The effects of dose, nutrition, and age on hexarelin-induced anterior pituitary hormone secretion in adult patients on maintenance hemodialysis. Journal of Clinical Endocrinology and Metabolism 84(4):1220-1225. PMID 10199757. DOI 10.1210/jcem.84.4.5635
- Tivesten Å, Bollano E, Caidahl K, Kujacic V, Sun XY, Hedner T, Hjalmarson Å, Bengtsson BÅ, Isgaard J (2000). The growth hormone secretagogue hexarelin improves cardiac function in rats after experimental myocardial infarction. Endocrinology 141(1):60-66. PMID 10614623. DOI 10.1210/endo.141.1.7249
- Cella SG, Cerri CG, Daniel S, Sibilia V, Rigamonti A, Cattaneo L, Deghenghi R, Müller EE (1996). Sixteen weeks of hexarelin therapy in aged dogs: effects on the somatotropic axis, muscle morphology, and bone metabolism. Journal of Gerontology A 51(6):B439-B447. PMID 8914494. DOI 10.1093/gerona/51a.6.b439
- Zhang G, Qu H, Chen G, Chen W (2018). Improvement of cardiomyocyte function by in vivo hexarelin treatment in streptozotocin-induced diabetic rats. Physiological Reports 6(3):e13612. PMID 29446246. DOI 10.14814/phy2.13612
- Dominikowski A, Rękoś M, Olejarz W, Szczepanek-Parulska E, Domin R, Ruchała M (2026). The emerging landscape of performance-enhancing peptides modulating the GH-IGF1 axis: bridging the gap between clinical evidence and patient self-administration. Frontiers in Endocrinology 17:1822475. PMID 42395176. DOI 10.3389/fendo.2026.1822475
- Annex to section 2(3) of the German Anti-Doping Act (AntiDopG), published at BGBl. 2023 I, No. 67, 1-5, section II.2.4, listing GHRP-2 (pralmorelin), GHRP-2-Gly, GHRP-6, GHRP-6-Gly and hexarelin. Full text read 10 September 2026. https://www.gesetze-im-internet.de/antidopg/anlage.html
- openFDA. Drug label endpoint, queries for substance names "hexarelin" and "examorelin", each returning HTTP 404, no matches; control query "semaglutide" returned 5 labels in the same run. Retrieved 10 September 2026. https://api.fda.gov/drug/label.json
- FDA. Bulk drug substances used in compounding under section 503A of the FD&C Act; full page text searched, no occurrence of hexarelin or examorelin. Retrieved 10 September 2026. https://www.fda.gov/drugs/human-drug-compounding/bulk-drug-substances-used-compounding-under-section-503a-fdc-act
- FDA. Certain bulk drug substances for use in compounding that may present significant safety risks; full page text searched, no occurrence of hexarelin or examorelin, against ten occurrences of ipamorelin as a positive control. Retrieved 10 September 2026. https://www.fda.gov/drugs/human-drug-compounding/certain-bulk-drug-substances-use-compounding-may-present-significant-safety-risks
- European Medicines Agency. Full-text medicines search attempted 10 September 2026; the site returned HTTP 401 and could not be searched. No European register finding of our own exists.
- MHRA. products.mhra.gov.uk returned only a JavaScript shell without a rendered result list on 10 September 2026, and the search interface behind it did not respond. No British register finding of our own exists.
- Health Canada. Drug Product Database, active ingredient API queries for "hexarelin" and "examorelin", 0 results each. Retrieved 10 September 2026. https://health-products.canada.ca/api/drug/activeingredient/?ingredientname=hexarelin
- State Register of Medicines of the Russian Federation (GRLS). Queries on 10 September 2026 returned empty result lists, including the control queries for semaglutide and Ozempic, so no finding can be drawn either way.
- Thomas A, Höppner S, Geyer H, Schänzer W, Petrou M, Kwiatkowska D, Pokrywka A, Thevis M (2011). Determination of growth hormone releasing peptides (GHRP) and their major metabolites in human urine for doping controls by means of liquid chromatography mass spectrometry. Analytical and Bioanalytical Chemistry 401(2):507-516. PMID 21298258. DOI 10.1007/s00216-011-4702-3
- Semenistaya E, Zvereva I, Thomas A, Thevis M, Krotov G, Rodchenkov G (2015). Determination of growth hormone releasing peptides metabolites in human urine after nasal administration of GHRP-1, GHRP-2, GHRP-6, hexarelin, and ipamorelin. Drug Testing and Analysis 7(10):919-925. PMID 25869809. DOI 10.1002/dta.1787
- openFDA. Drugs@FDA queries by generic name on 10 September 2026: "tesamorelin" returns BLA 022505, Theratechnologies, EGRIFTA; "cjc-1295" and "ibutamoren" return NOT_FOUND. https://api.fda.gov/drug/drugsfda.json
- Thomas A, Kohler M, Mester J, Geyer H, Schänzer W, Petrou M, Thevis M (2010). Identification of the growth-hormone-releasing peptide-2 (GHRP-2) in a nutritional supplement. Drug Testing and Analysis 2(3):144-148. PMID 20878896. DOI 10.1002/dta.120
Cite this page
The facts on this page were checked on 10 September 2026, and every register query behind the status table was run on that date. Nobody has developed hexarelin since the mid-2000s, so the regulatory and anti-doping entries are the parts most likely to change.
myPeptides Research & Editing. (2026). Hexarelin: what the studies show, status and safety. Version 1.0, 10 September 2026. myPeptides Peptide Register. Retrieved from https://mypep.app/peptides/hexarelin
How pages in this register are compiled and graded is described under methodology; the full register is at peptides.
| Version | Date | Change |
|---|---|---|
| 1.0 | 2026-09-10 | Initial publication |
Last verified: 10 September 2026. Next review: on any change to the anti-doping list, to the Australian Poisons Standard or to the FDA compounding lists, or on any new human study.